Drug testing lead candidate

Partly due to the limited throughput of Caco-2 permeability measurements, the structure-activity evaluation of compounds tested in the hit-to-lead phase is done with minimal permeability information, at best. Given the importance of membrane permeability in drug absorption, early consideration of the permeability characteristics of hit compounds would enhance the drug-like quality, and ultimately the probability of success, of selected lead candidates. To incorporate permeability information into the hit-to-lead phase of the drug discovery process it is necessary that permeability measurements be made quickly and with small amounts of material. Thus, efforts have been made to automate and miniaturize the Caco-2 permeability assay. 

Testing lead compounds and drug candidates for degradation by liver microsomes can inform a discovery team whether a compound suffers from significant first-pass metabolism. Animal testing also provides valuable early information on metabolic susceptibility. The real test, however, comes during clinical trials. Drugs that display an unfavorably... 

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